2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs c-Met/HGFR Apoptosis
  4. PROTAC c-Met degrader-6

PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC EGFR degrader 14 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: Target protein ligand: (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797), Target protein ligand + Linker (HY-175337)).

For research use only. We do not sell to patients.

PROTAC c-Met degrader-6

PROTAC c-Met degrader-6 Chemical Structure

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PROTAC c-Met degrader-6 Related Antibodies

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Description

PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC EGFR degrader 14 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: Target protein ligand: (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797), Target protein ligand + Linker (HY-175337))[1].

IC50 & Target[1]

c-Met

 

In Vitro

PROTAC c-Met degrader-6 (Compound G4) (72 h) exhibits antiproliferation efficacy with IC50 values of 3.55, 3.01, and 7.48 nM on EBC-1, Hs746T, and MHCC97H cells, respectively[1].
PROTAC c-Met degrader-6 (5-10 nM, 24-48 h) exhibits strong effects on inducing cell apoptosis, G1 cell cycle arrest, and inhibiting cell migration and invasion[1].
PROTAC c-Met degrader-6 (1-10 nM, 48 h) significantly degrades c-Met through the ubiquitin proteasome pathway in EBC-1 and Hs746T cells[1].
PROTAC c-Met degrader-6 (100-1000 nM, 48 h-3 days) exhibits excellent antiproliferative against EBC-1 and Hs746T cells with c-MetD1228N and c-MetY1230H mutants[1].
PROTAC c-Met degrader-6 exhibits good metabolic stability in the human liver microsome and mouse liver microsome[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC c-Met degrader-6 Related Antibodies

Apoptosis Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 10 nM
Incubation Time: 48 h
Result: Produced the apoptosis rates of 21.8% in EBC-1 and observed similar results in Hs746T.

Cell Cycle Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 10 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the G0/G1 phase.

Cell Migration Assay [1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 5 nM
Incubation Time: 24 h
Result: Significantly inhibited the migratory capacity.

Cell Invasion Assay[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 5 nM
Incubation Time: 24 h
Result: Significantly inhibited the invasive capacity.

Western Blot Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 1 and 10 nM
Incubation Time: 48 h
Result: Significantly inhibited the levels of c-Met phosphorylation (p-c-Met) and STAT3 phosphorylation (p-STAT3) at 1nM
Completely blocked the c-Met degradation effect pretreatment with MLN4924 (E1 ubiquitin-activating enzyme inhibitor) (HY-70062) and MG132 (proteasome inhibitor) (HY-13259).

Western Blot Analysis[1]

Cell Line: EBC-1 and Hs746T cells harboring a D1228N mutation
Concentration: 100 and 1000 nM
Incubation Time: 48 h
Result: Inhibited the p-c-Met level, and complete c-Met degradation and p-c-Met inhibition.
In Vivo

PROTAC c-Met degrader-6 (Compound G4) (5-10 mg/kg, p.o., once daily for 18 days) significantly inhibits tumor growth in EBC-1 xenografts mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: EBC-1 xenografts model established in NOD/SCID mice (6 week-old)[1]
Dosage: 5 and 10 mg/kg
Administration: Orally administration (p.o.), once daily for 18 days
Result: Significantly inhibited EBC-1 tumor growth, with tumor growth inhibition (TGI %) values of 84.12% at 5 mg/kg and 99.28% at 10 mg/kg after 10 days
Demonstrated complete tumor inhibition during the extended period (by day 18) at 10 mg/kg.
Exhibited a notable reduction in the percentage of Ki67-and CD31-positive tumor cells and an increased percentage of cleaved caspase 3-positive tumor cells.
Exhibited more potent effects on reducing the level of p-c-Met and p-STAT3.
No obvious body weight loss and no other obvious toxic signs.
Molecular Weight

749.77

Formula

C41H35N9O6
SMILES

O=C1NC(CCC1N(C(C2=CC(N3CCN(CC3)CCOC4=CN=C(N=C4)C5=CC=CC(CN6C(C=CC(C7=CC(C#N)=CC=C7)=N6)=O)=C5)=CC=C82)=O)C8=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC c-Met degrader-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC c-Met degrader-6PROTACsc-Met/HGFRApoptosisEBC-1 cellsHs746T cellsMHCC97H cellsXenograft mice modelPROTACInhibitorinhibitorinhibit

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